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Translational and Clinical Pharmacology Mar 2021Histamine acts by binding to four histamine receptors (H1 to H4), of which the H1 is known to participate in dilate blood vessels, bronchoconstriction, and pruritus....
UNLABELLED
Histamine acts by binding to four histamine receptors (H1 to H4), of which the H1 is known to participate in dilate blood vessels, bronchoconstriction, and pruritus. Olopatadine hydrochloride blocks the release of histamine from mast cells and it inhibits H1 receptor activation. Olopatadine hydrochloride is anti-allergic agent that is effectively used. The object of this study had conducted to compare the pharmacokinetics (PKs) and safety characteristics between olopatadine hydrochloride 5 mg (test formulation) and olopatadine hydrochloride 5 mg (reference formulation; Alerac ) in Korean subjects. This study had conducted an open-label, randomized, fasting condition, single-dose, 2-treatment, 2-period, 2-way crossover. Subjects received single-dosing of reference formulation or test formulation in each period and blood samples were collected over 24 hours after administration for PK analysis. A wash-out period of 7 days was placed between the doses. Plasma concentration of olopatadine were determined using liquid chromatography-tandem spectrometry mass (LC-MS/MS). A total of 32 subjects were enrolled and 28 subjects completed. There were not clinical significantly different in the safety between two treatment groups for 32 subjects who administered the study drug more than once. The geometric mean ratio of test formulation to reference formulation and its 90% confidence intervals for The peak plasma concentration (C) and the areas under the plasma concentration-time curve from 0 to the last concentration (AUC) were 1.0845 (1.0107-1.1637) and 1.0220 (1.0005-1.0439), respectively. Therefore, the test formulation was bioequivalent in PK characteristics and was equally safe as the reference formulation.
TRIAL REGISTRATION
Clinical Research Information Service Identifier: KCT0005943.
PubMed: 33855002
DOI: 10.12793/tcp.2021.29.e6 -
Indian Journal of Pharmacology 2020Vernal conjunctivitis comprises 0.5% of allergic eye diseases. The study is intended to collate the effectiveness of drugs by observing the reduction in signs and...
To evaluate the efficacy and safety of olopatadine 0.1% ophthalmic solution and bepotastine 1.5% ophthalmic solution in patients with vernal keratoconjunctivitis in a tertiary care hospital.
INTRODUCTION
Vernal conjunctivitis comprises 0.5% of allergic eye diseases. The study is intended to collate the effectiveness of drugs by observing the reduction in signs and symptoms.
OBJECTIVES
The objective of the study is to evaluate the effectiveness and safety of olopatadine 0.1% ophthalmic drops with bepotastine besilate 1.5% ophthalmic drops in patients with vernal keratoconjunctivitis (VKC).
MATERIALS AND METHODS
A randomized, open-label, comparative study conducted in Sarojini Devi Eye Hospital, Telangana. The study included 50 patients diagnosed with VKC, of which Group A and Group B were given olopatadine 0.1% ophthalmic drops and bepotastine besilate 1.5% ophthalmic drops, respectively, twice a day for 8 weeks. The reduction in signs and symptoms in both groups was compared. The observations and results were tabulated accordingly, and data were analyzed using the SPSS. The unpaired t-test is used as the test of significance in between two groups. P value is statistically significant when it is less than 0.05.
RESULTS
Overall, 50 cases were included in the study, 72% of total patients were in the age group of 5-10 years, and 28% were in the age group of 11-15 years. There were 39 males and 11 females. After 8 weeks of follow-up, the mean reduction in the scoring of symptoms and signs provided better and quicker relief of watering, ocular discomfort, and conjunctival hyperemia with bepotastine 1.5% eye drops. Olopatadine 0.1% eye drops provided faster improvement in papillary hypertrophy. Both drugs were equally effective in reducing itching. Laboratory findings of absolute eosinophil count had no statistical significance in between the two groups.
CONCLUSIONS
In this study, based on the evaluation of therapeutic performance, bepotastine eye drops proved quicker relief of symptoms and signs compared to olopatadine eye drops but was not statistically significant which would prove beneficial for the patients.
Topics: Adolescent; Child; Child, Preschool; Conjunctivitis, Allergic; Female; Humans; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Piperidines; Pyridines; Tertiary Care Centers; Treatment Outcome
PubMed: 33666188
DOI: 10.4103/ijp.IJP_174_20 -
Indian Journal of Ophthalmology Feb 2021To compare the efficacy and safety of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2%, and Bepotastine besilate 1.5% ophthalmic solutions in the treatment of allergic... (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
To compare the efficacy and safety of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2%, and Bepotastine besilate 1.5% ophthalmic solutions in the treatment of allergic conjunctivitis.
METHODS
This is a prospective, observer-masked, comparative study of 180 patients with mild to moderate allergic conjunctivitis, randomized into three groups of 60 patients each. Each group was assigned to be treated with one of the three treatment options namely Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% ophthalmic solutions. Patients were followed-up at regular intervals with relief and resolution of symptoms and signs noted using Total Ocular Scoring System (TOSS) and hyperaemia scale.
RESULTS
All three topical medications were effective in resolving symptoms of the patients with mild to moderate allergic conjunctivitis. Baseline mean TOSS scores for Alcaftadine group, Olopatadine group and Bepotastine besilate group were (7.68±2.32), (7.65±2.32) and (7.45±2.27) respectively as compared to the corresponding TOSS scores on 14 Day (4 visit) which were (0.2 ± 0.43), (0.4 ± 0.56) and (0.1 ± 0.36) respectively. The resolution of symptoms in the Bepotastine and Alcaftadine groups was significantly profound as compared to the Olopatadine group (p = 0.008). Bepotastine and Alcaftadine groups significantly reduced allergic conjunctivitis symptoms compared to Olopatadine group (p = 0.008).
CONCLUSION
All three topical ophthalmic medications used in the study are safe and effective in the treatment of allergic conjunctivitis. However, Bepotastine and Alcaftadine appear to outweigh Olopatadine in resolving the symptoms of allergic conjunctivitis.
Topics: Anti-Allergic Agents; Benzazepines; Conjunctivitis, Allergic; Double-Blind Method; Humans; Imidazoles; Olopatadine Hydrochloride; Ophthalmic Solutions; Piperidines; Prospective Studies; Pyridines; Treatment Outcome
PubMed: 33463568
DOI: 10.4103/ijo.IJO_2083_20 -
Allergy, Asthma, and Clinical... 2020MP-AzeFlu is relatively new a pharmaceutical drug used in the treatment of allergic rhinitis. It is comprised of azelastine hydrochloride (AZE), a potent...
MP-AzeFlu is relatively new a pharmaceutical drug used in the treatment of allergic rhinitis. It is comprised of azelastine hydrochloride (AZE), a potent histamine-H1-receptor antagonist and fluticasone propionate (FP), corticosteroid. It's somewhat bitter taste (often considered a disadvantage) can be attributed to AZE. We here hypothesize that MP-AzeFlu may induce some of its beneficial effects through activation of bitter taste receptors (Tas2R), which have recently been described in human airways. In the nose Tas2Rs induce secretion of antimicrobial peptides and increase ciliary activity, while in the lung they cause airway smooth muscle relaxation. The mechanisms behind Tas2R-mediated effects are not yet fully known. In order to evaluate the role of Tas2R in the effects induced by MP-AzeFlu the dilatory response of pre-contracted isolated airways from Balb/c mice was investigated in tissue bath myographs in the presence or absence of various well-characterized pharmacological antagonists or their corresponding vehicles. MP-AzeFlu caused a potent dose-dependent relaxation of pre-contracted airways, an effect probably mediated by its AZE component. The dilatory effect of MP-AzeFlu and AZE both mimicked the response induced by the Tas2R agonist, chloroquine, but was independent of histamine receptor (H1-, H2- and H3-), prostaglandins, cAMP and cGMP involvement, all known to be common pathways for airway dilation. Other bitter-tasting antihistamines (i.e. olopatadine and desloratadine) also relaxed airway segments. These data support the notion that MP-AzeFlu has the ability to activate Tas2R in the same way as chloroquine. The effect appears to be mediated by AZE, but not via the histamine receptor. Activation of Tas2R by MP-AzeFlu may contribute to its superior efficacy over FP observed in controlled clinical trials in patients with moderate/severe allergic rhinitis.
PubMed: 32514276
DOI: 10.1186/s13223-020-00438-w -
Turkish Journal of Pharmaceutical... Dec 2019Forced degradation determines the intrinsic stability of a molecule by establishing degradation pathways in order to identify the likely degradation products (DPs). The...
OBJECTIVES
Forced degradation determines the intrinsic stability of a molecule by establishing degradation pathways in order to identify the likely degradation products (DPs). The objective of the present research was to establish intrinsic stability and forced degradation profiling of olopatadine hydrochloride.
MATERIALS AND METHODS
The intrinsic stability of olopatadine hydrochloride was evaluated by RP-HPLC, where a mixture of 0.1% formic acid and organic phase (methanol:acetonitrile; 50:50 % v/v) was used as mobile phase at 1.0 mL/min in gradient mode. Different stress conditions were employed to explore the intrinsic stability of olopatadine hydrochloride.
RESULTS
In acidic condition, five DPs, i.e. OLO1, OLO2, OLO3, OLO4, and OLO5, were observed. OLO5 was the major DP that increased with time and the peak area of OLO was decreased. In addition to OLO3 and OLO5, two more DPs were observed in alkaline condition, i.e. OLO6 and OLO7. OLO5 and OLO6 were two major DPs; OLO5 increased with time while OLO6 had a zigzag pattern of peak area with time. All DPs of neutral condition were also found in acidic condition while OLO3 and OLO5 were common in all three types of hydrolytic degradation.
CONCLUSION
Thus, OLO has similar pattern of degradation profiling in all hydrolytic conditions (acidic, alkaline, and neutral). No degradation was found in thermal, ultraviolet light, or oxidative conditions over 10 days. OLO-Imp was recognized as an analogue structure of OLO and proposed as 11-[(3-dimethylamino)-propylidene]-6,11-dihydro-dibenz[b,e]oxepin-2-propanoic acid in standard drug. OLO1 was identified as (2-(4-(dimethylamino) butyl) phenyl)methanol, which may be formed by cleavage of the tricyclic ring in neutral condition.
PubMed: 32454741
DOI: 10.4274/tjps.galenos.2018.83007 -
Journal of Investigational Allergology... Feb 2020
Topics: Child, Preschool; Drug Hypersensitivity; Drug-Related Side Effects and Adverse Reactions; Humans; Hypersensitivity, Immediate; Infant; Male; Olopatadine Hydrochloride; Polyethylene Glycols; Recurrence; Skin; Skin Tests
PubMed: 32077856
DOI: 10.18176/jiaci.0447 -
Medicine Feb 2020Allergic conjunctivitis (AC) is a multifactorial and common type of ocular surface disease that affects many people. The quality of life for AC patients can be...
BACKGROUND
Allergic conjunctivitis (AC) is a multifactorial and common type of ocular surface disease that affects many people. The quality of life for AC patients can be significantly decreased caused by symptoms of ocular itching, swelling, redness, and tearing. Topical antihistaminics, mast cell stabilizers, non-steroidal anti-inflammatory drugs (NSAIDs), and steroids have been widely used to treat AC. Many clinical trials have indicated that olopatadine hydrochloride eye drops can provide quick relief of symptoms and signs. The purpose of this review is to evaluate systematically the effectiveness of olopatadine hydrochloride eye drops for treating AC.
METHODS
A systematic review of all of the randomized controlled trials on the effectiveness and safety of olopatadine hydrochloride eye drops for AC will be conducted. We will search PubMed, Web of Science (WOS), EMBASE (OVID), the Cochrane Library, Google Scholar, China National Knowledge Infrastructure (CNKI), China Science and Technology Journal database (VIP), Wanfang Database, and CBM, from the database inception date to October 31, 2019. There are no language or publication status restrictions. Registers of clinical trials, potential gray literature, reference lists of studies, and conference abstracts will also be searched. Two reviewers will independently read the articles, extract the data information, and assess the quality of the studies. Data will be synthesized by a heterogeneity test. The primary outcomes include the main symptom and sign scores before and after treatment, the eye redness index, the presence of eosinophils in the conjunctival scraping. Quality of life, the total treatment efficacy, and safety will be evaluated as the secondary outcomes. RevMan V.5.3 software will be used for the meta-analysis.
RESULTS
The study will provide an objective and normative systematic review to evaluate the effectiveness and safety of olopatadine hydrochloride eye drops for the treatment of AC.
CONCLUSION
Our review will provide useful information to judge whether olopatadine hydrochloride eye drops is an effective intervention for patients with AC.
ETHICS AND DISSEMINATION
It is not necessary to obtain ethical approval as participants are not involved patients. The protocol and results will be published in a peer-reviewed journal. The systematic review will also be disseminated electronically and in print to help guide health care practice and policy.
PROSPERO REGISTRATION NUMBER
PROSPERO CRD42019132232.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Humans; Olopatadine Hydrochloride; Ophthalmic Solutions; Quality of Life; Randomized Controlled Trials as Topic; Treatment Outcome
PubMed: 32049778
DOI: 10.1097/MD.0000000000018618 -
Annals of Allergy, Asthma & Immunology... Feb 2020GSP301 is an investigational fixed-dose combination nasal spray of olopatadine hydrochloride (antihistamine) and mometasone furoate (corticosteroid). (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
GSP301 is an investigational fixed-dose combination nasal spray of olopatadine hydrochloride (antihistamine) and mometasone furoate (corticosteroid).
OBJECTIVE
To evaluate efficacy and safety of GSP301 in patients with seasonal AR (SAR).
METHODS
In this phase 2, double-blind, parallel-group study, patients (≥12 years of age) with SAR were equally randomized to twice-daily GSP301 (olopatadine 665 μg and mometasone 25 μg), once-daily GSP301 (olopatadine 665 μg and mometasone 50 μg), twice-daily or once-daily olopatadine monotherapy (665 μg), mometasone monotherapy (twice-daily 25 μg or once-daily 50 μg), or placebo for 14 days. The primary endpoint-mean change from baseline in morning and evening reflective Total Nasal Symptom Score (rTNSS)-was analyzed using analysis of covariance (ANCOVA; P < .05 = statistically significant). Average morning and evening 12-hour instantaneous TNSS (iTNSS), ocular symptoms, individual symptoms, onset of action, quality of life, and adverse events (AEs) were also assessed.
RESULTS
A total of 1111 patients were randomized. Twice-daily GSP301 provided statistically significant and clinically meaningful rTNSS improvements vs placebo (P < .001), twice-daily olopatadine (P = .049), and mometasone (P = .004). Similar significant improvements in iTNSS were observed with twice-daily GSP301 vs placebo (P < .001) and twice-daily mometasone (P = .007); improvements were not significant vs olopatadine (P = .058). Once-daily GSP301 provided significant rTNSS and iTNSS improvements vs placebo and once-daily olopatadine (P < .01, all) but improvements were not significant vs mometasone. Treatment-emergent AEs rates were 10.8%, 9.5%, and 8.2%, with twice-daily GSP301, once-daily GSP301, and placebo, respectively.
CONCLUSION
Twice-daily GSP301 treatment was efficacious and well tolerated, providing statistically significant and clinically meaningful improvements in rTNSS (primary endpoint) vs placebo and both monotherapies.
TRIAL REGISTRATION
Clinicaltrials.gov Identifier NCT02318303.
Topics: Drug Administration Schedule; Drug Combinations; Drug Therapy, Combination; Female; Humans; Male; Middle Aged; Mometasone Furoate; Nasal Sprays; Olopatadine Hydrochloride; Rhinitis, Allergic, Seasonal; Treatment Outcome
PubMed: 31734334
DOI: 10.1016/j.anai.2019.11.007 -
BMC Ophthalmology Nov 2019To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on...
BACKGROUND
To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on human corneal epithelial cells (HCECs) and their anti-allergic effects on cultured conjunctival epithelial cells.
METHODS
A Methylthiazolyltetrazolium(MTT)-based calorimetric assay was used to assess cytotoxicities using HCECs at concentrations of 10, 20 or 30% for exposure durations of 30 min, 1 h, 2 h, 12 h or 24 h. Cellular morphologies were evaluated by inverted phase-contrast and electron microscopy. Wound widths were measured 2 h, 18 h, or 24 h after confluent HCECs monolayers were scratched. Realtime PCR was used to quantify anti-allergic effects on cultured human conjunctival cells, in which allergic reactions were induced by treating them with Aspergillus antigen.
RESULTS
Cell viabilities decreased in time- and concentration-dependent manners. Cells were detached from dishes and showed microvilli loss, cytoplasmic vacuoles, and nuclear condensation when exposed to antiallergic agents; alcaftadine was found to be least cytotoxic. Alcaftadine treated HCECs monolayers showed the best wound healing followed by bepotastine and olopatadine (p < 0.0001). All agents significantly reduced the gene expressions of allergic cytokines (IL-5, IL-25, eotaxin, thymus and activation-regulated chemokine, and thymic stromal lymphopoietin) and alcaftadine had the greatest effect (p < 0.0001 in all cases).
CONCLUSIONS
Alcaftadine seems to have less side effects and better therapeutic effects than the other two anti-allergic agents tested. It may be more beneficial to use less toxic agents for patients with ocular surface risk factors or presumed symptoms of toxicity.
Topics: Anti-Allergic Agents; Benzazepines; Cell Survival; Cells, Cultured; Conjunctiva; Cornea; Epithelial Cells; Humans; Imidazoles; Olopatadine Hydrochloride; Piperidines; Pyridines
PubMed: 31703568
DOI: 10.1186/s12886-019-1228-5 -
Indian Journal of Ophthalmology Sep 2019With increasing environmental pollution, the incidence of allergic conjunctivitis is increasing. Newer anti-allergic medications with combined anti-histaminic and mast... (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
With increasing environmental pollution, the incidence of allergic conjunctivitis is increasing. Newer anti-allergic medications with combined anti-histaminic and mast cell stabilization action can help reducing the use of topical steroids for milder form of disease. There is no study directly comparing olopatadine (0.1%), bepotastine (1.5%), and alcaftadine (0.25%) for mild to moderate allergic conjunctivitis cases. Hence, we decided to methodically study the efficacy of three topical medications.
METHODS
Prospective, observer-masked clinical trial enrolled 45 patients with 15 patients in each of the three groups. Patients with mild to moderate allergic conjunctivitis were sequentially assigned to respective groups, and relief of symptoms and signs were noted upto 1-month follow-up.
RESULTS
All three topical medications faired almost equally in resolving symptoms of the patients with mild to moderate allergic conjunctivitis, and most of them reported complete relief after 1 week of use of medication. Few cases with limbal or palpebral papillae reported symptomatic relief after use of medication, but the resolution of these signs was not noted in all three groups.
CONCLUSION
We concluded similar efficacy of three medications in relieving symptoms and inefficacy in regressing palpebral and limbal papillae in cases of allergic conjunctivitis.
Topics: Adolescent; Adult; Anti-Allergic Agents; Benzazepines; Child; Conjunctiva; Conjunctivitis, Allergic; Dose-Response Relationship, Drug; Female; Follow-Up Studies; Histamine H1 Antagonists; Humans; Imidazoles; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Piperidines; Prospective Studies; Pyridines; Single-Blind Method; Treatment Outcome; Young Adult
PubMed: 31436181
DOI: 10.4103/ijo.IJO_2112_18